Synthesis and biological activity of some Val (Ala) -Tyr and Val-Tyr-Tyr peptides
Chen, P.L.; Peng, S.X.; Yang, Z.X.
Yao Xue Xue Bao 27(12): 895-902
1992
ISSN/ISBN: 0513-4870 PMID: 1299138 Document Number: 398000
I5B2 and WF-10129, reported as potent angiotensin-converting enzyme inhibitors (ACEI), were used as lead compounds for design of novel ACEI. Some of Val-Tyr-Tyr and Val-Tyr peptides were synthesized and tested for ability to inhibit ACE in vitro and in vivo. The most potent compound was found to be N-(1-,benzoyl-1-carboxylmethyl)-L-Alayl-L-Tyrosine (II-5, IC-50=7.9 times 10-10 mol/L) which was prepared by the addition of Ala-Tyr to benzoylacrylic acid in the presence of triethylamine. The structure-activity relationships were also discussed.